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Target
Metabotropic glutamate receptor 8
Ligand
BDBM50283491
Substrate
n/a
Meas. Tech.
ChEMBL_1725550 (CHEMBL4140828)
EC50
900±n/a nM
Citation
 Abe, M; Seto, M; Gogliotti, RG; Loch, MT; Bollinger, KA; Chang, S; Engelberg, EM; Luscombe, VB; Harp, JM; Bubser, M; Engers, DW; Jones, CK; Rodriguez, AL; Blobaum, AL; Conn, PJ; Niswender, CM; Lindsley, CW Discovery of VU6005649, a CNS Penetrant mGlu ACS Med Chem Lett 8:1110-1115 (2017) [PubMed]  Article 
Target
Name:
Metabotropic glutamate receptor 8
Synonyms:
GRM8_RAT | Gprc1h | Grm8 | Metabotropic glutamate receptor | Metabotropic glutamate receptor 8 (mGlu8) | Mglur8 | glutamate receptor, metabotropic 8 precursor | mGlu8 | metabotropic glutamate 8
Type:
Enzyme
Mol. Mass.:
101886.18
Organism:
Rattus norvegicus (Rat)
Description:
P70579
Residue:
908
Sequence:
MVCEGKRLASCPCFFLLTAKFYWILTMMQRTHSQEYAHSIRVDGDIILGGLFPVHAKGERGVPCGELKKEKGIHRLEAMLYAIDQINKDPDLLSNITLGVRILDTCSRDTYALEQSLTFVQALIEKDASDVKCANGDPPIFTKPDKISGVIGAAASSVSIMVANILRLFKIPQISYASTAPELSDNTRYDFFSRVVPPDSYQAQAMVDIVTALGWNYVSTLASEGNYGESGVEAFTQISREIGGVCIAQSQKIPREPRPGEFEKIIKRLLETPNARAVIMFANEDDIRRILEAAKKLNQSGHFLWIGSDSWGSKIAPVYQQEEIAEGAVTILPKRASIDGFDRYFRSRTLANNRRNVWFAEFWEENFGCKLGSHGKRNSHIKKCTGLERIARDSSYEQEGKVQFVIDAVYSMAYALHNMHKERCPGYIGLCPRMVTIDGKELLGYIRAVNFNGSAGTPVTFNENGDAPGRYDIFQYQINNKSTEYKIIGHWTNQLHLKVEDMQWANREHTHPASVCSLPCKPGERKKTVKGVPCCWHCERCEGYNYQVDELSCELCPLDQRPNINRTGCQRIPIIKLEWHSPWAVVPVFIAILGIIATTFVIVTFVRYNDTPIVRASGRELSYVLLTGIFLCYSITFLMIAAPDTIICSFRRIFLGLGMCFSYAALLTKTNRIHRIFEQGKKSVTAPKFISPASQLVITFSLISVQLLGVFVWFVVDPPHTIIDYGEQRTLDPENARGVLKCDISDLSLICSLGYSILLMVTCTVYAIKTRGVPETFNEAKPIGFTMYTTCIIWLAFIPIFFGTAQSAEKMYIQTTTLTVSMSLSASVSLGMLYMPKVYIIIFHPEQNVQKRKRSFKAVVTAATMQSKLIQKGNDRPNGEVKSELCESLETNTSSTKTTYISYSNHSI
  
Inhibitor
Name:
BDBM50283491
Synonyms:
CHEMBL1585091
Type:
Small organic molecule
Emp. Form.:
C24H24N2O4S
Mol. Mass.:
436.523
SMILES:
COC(=O)c1ccc(cc1)-n1c(C)cc(C(=O)CSc2ccc(NC(C)=O)cc2)c1C
Structure:
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